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Active ingredients
Azithromycin
Release form
Capsules
Composition
1 capsule contains: Active substance: azithromycin dihydrate in terms of azithromycin - 250 mg. Excipients: mannitol (mannitol) - 54.58 mg, corn starch - 13.10 mg, magnesium stearate - 2.0 mg, sodium lauryl sulfate - 0.32 mg, Hard gelatin capsules composition capsules: body and cap - titanium dioxide ( E 171), gelatin (medical gelatin).
Pharmacological effect
A broad-spectrum antibiotic, a representative of the macrolide antibiotic subgroup - azalides. By binding to the 50S subunit of ribosomes, it inhibits peptide translocation at the translation stage, inhibits protein synthesis, slows the growth and reproduction of bacteria. It acts bacteriostatic, in high concentrations has a bactericidal effect. Acts on extracellular and intracellular pathogens. Active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Streptococcus viridans, Staphylococcus aureus; Gram negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; Some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp., as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Azithromycin is not active against gram-positive bacteria that are resistant to erythromycin.
Pharmacokinetics
Absorption: After taking the drug inside azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. After oral administration, 500 mg of azithromycin Cmax in plasma is reached in 2.5-3 hours and is 0.4 mg / l. Bioavailability - 37%. Taking the drug simultaneously with food slows down and reduces the absorption of azithromycin. Distribution: Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate gland), skin and soft tissues. High tissue concentrations (10–50 times higher than in plasma) and prolonged T1 / 2 are due to the low binding of azithromycin to plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding the lysosomes. This, in turn, determines a large apparent Vd (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate primarily in lysosomes is especially important for the elimination of intracellular pathogens.It has been proven that phagocytes deliver azithromycin to the site of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (by an average of 24–34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function. Azithromycin remains in bactericidal concentrations in the inflammatory focus for 5–7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment. Metabolism: In the liver, azithromycin is demethylated, the resulting metabolites are inactive. Removal: Removal of azithromycin from blood plasma takes place in 2 stages: T1 / 2 is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours, which allows you to use the drug 1 time / day .
Indications
Infectious and inflammatory diseases caused by microorganisms susceptible to the drug: Infections of the upper respiratory tract and upper respiratory tract (including angina, sinusitis, tonsillitis, otitis media). Scarlet fever. Infections of the lower respiratory tract (including bacterial and atypical pneumonia, bronchitis). Infections of the skin and soft tissues (including Erysipelas, impetigo, secondarily infected dermatosis). Infections of the urogenital tract (including Urethritis and / or cervicitis). Lyme disease (borreliosis) in the initial stage (erythema migrans) .Diseases of the stomach and twelve atyptic bowel associated with helicobacter pylori (as part of combination therapy).
Contraindications
Hepatic insufficiency. Renal failure. Children weighing less than 45 kg (for 500 mg capsules). Children up to 12 years old. Increased sensitivity to antibiotics of the macrolide group. Use caution when using the drug for arrhythmias (ventricular arrhythmias are possible, lengthening the interval), children with severe impaired liver or kidney function.
Precautionary measures
The drug should be used with caution in case of arrhythmia (ventricular arrhythmias are possible, prolongation of the QT interval) in children with severe disorders of the liver or kidneys.
Use during pregnancy and lactation
The use of the drug during pregnancy is possible only in the case when the intended benefits to the mother outweigh the potential risk to the fetus.If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.
Dosage and administration
Azitrox taken orally 1 time / day for 1 hour before or 2 hours after eating. Adults with upper and lower respiratory tract infections are prescribed 500 mg / day for 3 days (a course dose of 1.5 g). With infections of the skin and soft tissues, it is prescribed in a dose of 1 g / day for 1 dose on the first day, then - 500 mg / day daily from 2 to 5 days. Course dose - 3 g. With uncomplicated urethritis and / or cervicitis, 1 g is prescribed once. With a complicated, long-lasting urethritis / cervicitis caused by Chlamydia trachomatis, 1 g 3 times with an interval of 7 days (taking the drug in 1-7 14 day treatment). Course dose - 3 g. In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), 1 g is prescribed on the 1st day and 500 mg daily from the 2nd to the 5th day. The course dose is 3 g. For gastric ulcer and duodenal ulcer associated with Helicobacter pylori, 1 g / day is prescribed for 3 days as part of combination anti-helicobacter therapy. Children with a body weight of more than 45 kg with infections of the upper and lower respiratory tract, skin and soft tissues, scarlet fever, the drug is prescribed at 500 mg / day (1 capsule) per 1 intake for 3 days. For children over 12 years old, the drug (capsules 250 mg) is prescribed at the rate of 10 mg / kg 1 time / day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day within 3 days. Heading dose - 30 mg / kg. In the treatment of erythema migrans in children, the dose of the drug (caps. 500 mg) is 1 g on the 1st day and 500 mg daily from the 2nd to the 5th day. The course dose is 3 g. Azitrox in the form of capsules of 250 mg should be used in a dose of 20 mg / kg on the 1st day and 10 mg / kg - from the 2nd to the 5th day.
Side effects
On the part of the digestive system, diarrhea (5%), nausea (3%), abdominal pain (3%). 1% - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases. children have constipation, anorexia, gastritis. Candidomycosis of the oral mucosa is possible. From the side of the cardiovascular system there is a feeling of palpitations, pain in the chest (≤1%). From the side of the central nervous system dizziness, headache, drowsiness. in children - headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disorders (≤1%). On the part of the reproductive system ≤1% - vaginal candidiasis. Of the urinary system ≤1% - nephritis. Dermatological reactions in in some cases - rash, photosensitization. Allergic reactions rash, itching, angioedema, urticaria, conjunctivitis. Others have increased fatigue.
Overdose
Symptoms: with the use of the drug in high doses may increase side effects - severe nausea, temporary hearing loss, vomiting, diarrhea. Treatment: gastric lavage, the appointment of activated carbon, conducting symptomatic therapy.
Interaction with other drugs
Antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin. Azithromycin is not associated with cytochrome P450 isoenzymes. Unlike most macrolides, azithromycin does not interact with theophylline, terfenadine, carbamazepine, triazolam, digoxin. Macrolides (except azalides) slow excretion and increase plasma concentrations and toxicity of cycloserine, anticoagulants, methylprednisolone, felodipine, as well as preparations suffer from microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproate, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline), due to inhibition of microsomal oxidation in hepatocytes, while azalides such interaction to date have been noted. With simultaneous use of azithromycin with digoxin, an increase in the concentration of the latter is observed. With simultaneous administration of warfarin and azithromycin (in usual doses), no changes in the prothrombin time have been identified, however, given that the interaction of macrolides and warfarin may increase the anticoagulant effect, patients need careful control of the prothrombin time. With simultaneous use of azithromycin with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) is enhanced. With the simultaneous use of azithromycin with triazolam, the clearance is reduced and the pharmacological action of triazolam is enhanced. Lincosamines reduce the effectiveness of azithromycin. Tetracycline and chloramphenicol enhance the effectiveness of azithromycin. Pharmaceutical incompatibility: Azithromycin is pharmaceutically incompatible with heparin.
special instructions
Azitrox should not be taken with food.In the case of skipping the next dose, the missed dose should be taken as quickly as possible, and the next - with an interval of 24 hours. A break of at least 2 hours should be observed between taking Azitrox and antacids. After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under medical supervision.